Drug intelligence / Profile preview

tirzepatide + oral antihyperglycemic medication

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Peptides, Small Molecules
Administration
Subcutaneous, Oral
01

Overview

Tirzepatide is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist developed by Eli Lilly. This therapeutic regimen involves the use of tirzepatide as an add-on therapy to one or more oral antihyperglycemic medications (OAMs), such as metformin, SGLT2 inhibitors, or sulfonylureas. Tirzepatide is a 39-amino acid synthetic peptide that mimics the actions of endogenous GIP and GLP-1, enhancing glucose-dependent insulin secretion, suppressing glucagon levels, and slowing gastric emptying. In clinical trials such as the SURPASS-4 and SURPASS J-combo studies, the addition of tirzepatide to background OAM therapy demonstrated superior glycemic control (HbA1c reduction) and significant body weight loss compared to OAMs alone or other injectable comparators like insulin glargine. It is FDA-approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Brand names
Mounjaro
Other names
tirzepatide plus OAMtirzepatide add-on to oral antihyperglycemic medications
02

Targets

GLP1R (GLP-1R)GIPR (Gastric inhibitory polypeptide receptor)

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